- SUBSTITUTED SULFONE-CONTAINING TRICYCLIC COMPOUNDS AND USES THEREOF
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The present invention relates to substituted sulfone-containing tricyclic compounds and analogues thereof which inhibit Bak-mediated apoptosis. The invention further relates to pharmaceutical compositions comprising a compound of the present invention and to methods of inhibiting a Bak-mediated apoptotic pathway and Bak-mediated apoptosis in a cell.
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Page/Page column 27; 28
(2014/05/24)
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- Synthesis and biochemical evaluation of thiochromanone thiosemicarbazone analogues as inhibitors of cathepsin L
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A series of 36 thiosemicarbazone analogues containing the thiochromanone molecular scaffold functionalized primarily at the C-6 position were prepared by chemical synthesis and evaluated as inhibitors of cathepsins L and B. The most promising inhibitors f
- Song, Jiangli,Jones, Lindsay M.,Kumar, G. D. Kishore,Conner, Elizabeth S.,Bayeh, Liela,Chavarria, Gustavo E.,Charlton-Sevcik, Amanda K.,Chen, Shen-En,Chaplin, David J.,Trawick, Mary Lynn,Pinney, Kevin G.
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supporting information; experimental part
p. 450 - 453
(2012/09/25)
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- Synthesis and antitumor activities of a new series of 4,5-dihydro-1H- thiochromeno[4,3-d]pyrimidine derivatives
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A new series of 4,5-dihydro-1H-thiochromeno[4,3-d ]pyrimidine derivatives have been designed and synthesized. The antitumor activities of the target compounds have been evaluated in vitro against two human cancer cell lines including A549 (human alveolar adenocarcinoma cell) and H460 (human lung cancer) by MTT assay. Most of the target compounds exhibited significant antitumor activities against A549 and H460 cancer cell lines. The most potent compound 4-(benzo[d][1,3]dioxol-5-yl)-8,9-difluoro-2-(4-methylpiperazin-1-yl)-4, 5-dihydro-1H-thiochromeno[4,3-d]pyrimidine (CH05) (IC50 = 0.44 μM, 3.07 μM) was 2.0 and 8.4 times more active than gefitinib (IC50 = 0.89 μM, 16.81 μM) against A549 and H460 cell lines, respectively.
- Guo, Dexiang,Liu, Yajing,Li, Ting,Wang, Nan,Zhai, Xin,Hu, Chun,Gong, Ping
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experimental part
p. 347 - 351
(2012/08/08)
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